GDC-0349 - 10mM in DMSO , Serine/threonine-protein kinase mTOR inhibitor, CAS No.1207360-89-1, Serine/threonine-protein kinase mTOR inhibitor

CAS: 1207360-89-1 Cat. No.: G407793 Formula: C₂₄H₃₂N₆O₃ Molecular Weight: 452.55

GRADE & PURITY 10mM in DMSO

Synonyms

RG-7603 | Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

GDC-0349 GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
In vitro

GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes.

In vivo

GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN ) and 786-O (VHL mutant).
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

RG-7603 | Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]-

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K_i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Serine/threonine-protein kinase mTOR inhibitor

Names and Identifiers

• Isomeric SMILES: CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4COC4)C(=N2)N5CCOC[C@@H]5C
• Molecular Weight: 452.55
• Reaxy-Rn: 52178663
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=52178663&ln=

Associated Targets(Human)

MTOR Tclin Serine/threonine-protein kinase mTOR (2 Activities)

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Frequently Asked Questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1207360-89-1, the molecular formula is C24H32N6O3, and the molecular weight is 452.55 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.